Targeting Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2): Latest Insights on Synthetic Strategies
Vascular endothelial growth factor receptor 2 (VEGFR-2) is a crucial mediator of angiogenesis, playing a pivotal role in both normal physiological processes and cancer progression. Tumors harness VEGFR-2 signaling to promote abnormal blood vessel growth, which is a key step in the metastasis process...
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MDPI AG
2024-11-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/29/22/5341 |
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| author | Carolina S. Marques Pedro Brandão Anthony J. Burke |
| author_facet | Carolina S. Marques Pedro Brandão Anthony J. Burke |
| author_sort | Carolina S. Marques |
| collection | DOAJ |
| description | Vascular endothelial growth factor receptor 2 (VEGFR-2) is a crucial mediator of angiogenesis, playing a pivotal role in both normal physiological processes and cancer progression. Tumors harness VEGFR-2 signaling to promote abnormal blood vessel growth, which is a key step in the metastasis process, making it a valuable target for anticancer drug development. While there are VEGFR-2 inhibitors approved for therapeutic use, they face challenges like drug resistance, off-target effects, and adverse side effects, limiting their effectiveness. The quest for new drug candidates with VEGFR-2 inhibitory activity often starts with the selection of key structural motifs present in molecules currently used in clinical practice, expanding the chemical space by generating novel derivatives bearing one or more of these moieties. This review provides an overview of recent advances in the development of novel VEGFR-2 inhibitors, focusing on the synthesis of new drug candidates with promising antiproliferative and VEGFR-2 inhibition activities, organizing them by relevant structural features. |
| format | Article |
| id | doaj-art-e28f374adca448e5bded00e1fc31f52a |
| institution | OA Journals |
| issn | 1420-3049 |
| language | English |
| publishDate | 2024-11-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj-art-e28f374adca448e5bded00e1fc31f52a2025-08-20T02:05:06ZengMDPI AGMolecules1420-30492024-11-012922534110.3390/molecules29225341Targeting Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2): Latest Insights on Synthetic StrategiesCarolina S. Marques0Pedro Brandão1Anthony J. Burke2LAQV-REQUIMTE, Institute for Research and Advanced Training, University of Évora, Rua Romão Ramalho, 59, 7000-641 Evora, PortugalEgas Moniz Center for Interdisciplinary Research (CiiEM), Egas Moniz School of Health & Science, Campus Universitátio, Quinta da Granja, Monte da Caparica, 2829-511 Caparica, PortugalCentro de Química de Coimbra, Institute of Molecular Sciences (CQC-IMS), Departamento de Química, Faculdade de Ciências e Tecnologia, University of Coimbra, 3004-535 Coimbra, PortugalVascular endothelial growth factor receptor 2 (VEGFR-2) is a crucial mediator of angiogenesis, playing a pivotal role in both normal physiological processes and cancer progression. Tumors harness VEGFR-2 signaling to promote abnormal blood vessel growth, which is a key step in the metastasis process, making it a valuable target for anticancer drug development. While there are VEGFR-2 inhibitors approved for therapeutic use, they face challenges like drug resistance, off-target effects, and adverse side effects, limiting their effectiveness. The quest for new drug candidates with VEGFR-2 inhibitory activity often starts with the selection of key structural motifs present in molecules currently used in clinical practice, expanding the chemical space by generating novel derivatives bearing one or more of these moieties. This review provides an overview of recent advances in the development of novel VEGFR-2 inhibitors, focusing on the synthesis of new drug candidates with promising antiproliferative and VEGFR-2 inhibition activities, organizing them by relevant structural features.https://www.mdpi.com/1420-3049/29/22/5341VEGFR-2inhibitors5-member heterocycle6-member heterocyclecoumarinisatin |
| spellingShingle | Carolina S. Marques Pedro Brandão Anthony J. Burke Targeting Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2): Latest Insights on Synthetic Strategies Molecules VEGFR-2 inhibitors 5-member heterocycle 6-member heterocycle coumarin isatin |
| title | Targeting Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2): Latest Insights on Synthetic Strategies |
| title_full | Targeting Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2): Latest Insights on Synthetic Strategies |
| title_fullStr | Targeting Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2): Latest Insights on Synthetic Strategies |
| title_full_unstemmed | Targeting Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2): Latest Insights on Synthetic Strategies |
| title_short | Targeting Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2): Latest Insights on Synthetic Strategies |
| title_sort | targeting vascular endothelial growth factor receptor 2 vegfr 2 latest insights on synthetic strategies |
| topic | VEGFR-2 inhibitors 5-member heterocycle 6-member heterocycle coumarin isatin |
| url | https://www.mdpi.com/1420-3049/29/22/5341 |
| work_keys_str_mv | AT carolinasmarques targetingvascularendothelialgrowthfactorreceptor2vegfr2latestinsightsonsyntheticstrategies AT pedrobrandao targetingvascularendothelialgrowthfactorreceptor2vegfr2latestinsightsonsyntheticstrategies AT anthonyjburke targetingvascularendothelialgrowthfactorreceptor2vegfr2latestinsightsonsyntheticstrategies |